Abstract
Liposome is a promising carrier system for delivering bioactive molecules. However, the successful delivery of pH-sensitive molecules is still limited by the intrinsic instability of payloads in physiological environment. Herein, we developed a special liposome system that possesses an acidic micro-environment in the internal aqueous chamber to improve the chemical stability of pH-sensitive payloads. Curcumin-loaded liposomes (Cur-LPs) with varied internal pH values (pH 2.5, 5.0, or 7.4) were prepared. These Cur-LPs have similar particle size of 300 nm, comparable physical stabilities and analogous in vitro release profiles. Interestingly, the chemical stability of liposomal curcumin in 50% fetal bovine serum and its anticancer efficacy in vitro are both micro-environmental pH-dependent (Cur-LP-2.5 > Cur-LP-5.0 > Cur-LP-7.4). This serum stability still has space to be further enhanced to improve the applicability of Cur-LP. In conclusion, creating an acidic micro-environment in the internal chamber of liposome is feasible and efficient to improve the chemical stability of pH-sensitive payloads.
Highlights
Liposome, an artificial membrane vehicle, has shown great potentials in drug delivery due to its drug loading capacity, biodegradability, and biocompatibility [1,2,3,4]
Characterization of Liposome The micro-environmental pH of liposome refers to the acidity in the inner aqueous chamber of liposome (Fig. 1), which is different from the pH in the external environment
The transmittance change of all the three LPs was less than 10% (Fig. 4b), indicating little particle sedimentation and a high kinetic stability. These results suggest that the three LPs have an excellent colloidal stability within 72 h, and the micro-environmental pH has no influence on physical stability of liposome
Summary
An artificial membrane vehicle, has shown great potentials in drug delivery due to its drug loading capacity, biodegradability, and biocompatibility [1,2,3,4]. The classic liposome is similar with living cells in structure, typically consisting of a phospholipid bilayer and an aqueous inner chamber [5,6,7] Due to this structure, liposome is able to solubilize the insoluble drug molecules and prevent the loaded drug from the harsh physiological environment [8,9,10]. Liposome has an aqueous space in its inner chamber, which can be used to provide drug payloads with an acidic micro-environment (Fig. 1) In this present work, we use curcumin as a model drug and aim to provide a novel approach for enhancing the chemical stability of drug molecules loaded in liposome. Curcumin is a suitable model drug for this work
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